摘要：

Naturally occurring novel bioactive microbial metabolites have been discovered by a variety of customized screening methods in the Kitasato Institute, which have been promising to subsequently develop into novel and extremely useful pharmaceutical products. This chapter provides an overview of this research, encompassing the isolation, the total synthesis, and the analogue synthesis as well as the determination of the absolute stereochemistry of bioactive microbial metabolites, such as pyripyropenes (cholesterol lowering agents), arisugacins (acetylcholinesterase inhibitors), lactacystin (proteasome inhibitor), macrosphelides (cell-cell adhesion inhibitors), madindolines (IL-6 modulators), and neoxaline (cell proliferation inhibitor).

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